ELN318463 racemate|851599-82-1|-陌孚医药/Medlife

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ELN318463 racemate

目录号: PL13301

CAS No. :851599-82-1

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中文名称	ELN318463 racemate
中文别名	化合物 T11178L
英文名称	ELN318463 racemate
英文别名	ELN 318463 (racemate);ELN318463 racemate;ELN-318463 racemate;N-[(4-bromophenyl)methyl]-4-chloro-N-(2-oxoazepan-3-yl)benzenesulfonamide;Benzenesulfonamide, N-[(4-bromophenyl)methyl]-4-chloro-N-(hexahydro-2-oxo-1H-azepin-3-yl)-
Cas No.	851599-82-1
分子式	C₁₉H₂₀BrClN₂O₃S
分子量	471.80
包装储存	Please store the product under the recommended conditions in the Certificate of Analysis.

产品详情	ELN318463 racemate 是 ELN318463 的外消旋体。ELN318463 是淀粉样前体蛋白 (APP) 选择性的 γ-分泌酶 (γ-secretase) 抑制剂。ELN318463 对包含早老蛋白 (PS1) 和 PS2 的 γ-分泌酶抑制活性不同，对 PS1 和 PS2 的 EC₅₀ 分别为 12 nM 和 656 nM。ELN318463 对 PS1 的选择性比对 PS2 高约 51 倍。
生物活性	ELN318463 racemate is the racemate of ELN318463. ELN318463 is an amyloid precursor protein (APP) selective γ-secretase inhibitor. ELN318463 shows differential inhibition of presenilin (PS1)- and PS2-comprised γ-secretase with EC 50 s of 12nM and 656 nM for PS1and PS2, respectively. ELN318463 is 51-fold more selective for PS1.
IC50 & Target[1][2]	γ-secretase
体外研究(In Vitro)	ELN318463 behaves as a classic γ-secretase inhibitor, demonstrates 75- to 120-fold selectivity for inhibiting Aβ production compared with Notch signaling in cells, and displaces an active site directed inhibitor at very high concentrations only in the presence of substrate. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	Brain levels of ELN318463 at 30 mg/kg are 0.754 μM in FVB brains and 0.69 μM in PDAPP brains, and at 100 mg/kg dose the levels were 2.7 μM in FVB brains and 1.87 μM in PDAPP brains. Discordance between Aβ 1-40 and Aβ x-40 in BACE KO or wild-type BACE inhibitor treated mice has been reported. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献	[1]. Zhao B, et al. Identification of gamma-secretase inhibitor potency determinants on presenilin. J Biol Chem. 2008 Feb 1;283(5):2927-38. [2]. Basi GS, et al. Amyloid precursor protein selective gamma-secretase inhibitors for treatment of Alzheimers disease. Alzheimers Res Ther. 2010 Dec 29;2(6):36.

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